磺化二膦(L)和环糊精(CD)的组合可以制备非常稳定的水溶性钌纳米粒子(RuNPs),该纳米粒子在不饱和底物的氢化反应中表现出相关的催化性能,并且具有环糊精的超分子控制作用。为了进行比较,通过在温和的条件下(3 bar H 2)氢化有机金属[Ru(1,5-环辛二烯)(1,3,5-环辛三烯)]络合物生成RuNP; 室温下),并在存在L或L / CD混合物作为稳定剂的情况下分别产生Ru / L和Ru / L / CD系统。如此获得的纳米颗粒通过互补技术得到了充分表征。有趣的是,NMR研究证明1)磺化二膦配体在金属表面上的强配位作用; 2)在环糊精存在下,L和CD之间形成包合物,改变了二膦的配位方式。对两个不饱和底物进行双相加氢的RuNPs体系的研究指出了反应性方面的相关差异,从而证明了金属表面上的超分子相互作用对纳米催化剂催化性能的影响。
A compound represented by formula (I) having mTOR inhibitory activity or a pharmacologically acceptable salt thereof.
具有mTOR抑制活性的公式(I)表示的化合物或其药理可接受的盐。
[EN] INHIBITORS OF INDOLEAMINE 2,3-DIOXYGENASE AND/OR TRYPTOPHAN 2,3-DIOXYGENASE<br/>[FR] INHIBTEURS DE L'INDOLÉAMINE 2,3-DIOXYGÉNASE ET/OU DU TRYPTOPHANE DIOXYGÉNASE
申请人:IDORSIA PHARMACEUTICALS LTD
公开号:WO2019034725A1
公开(公告)日:2019-02-21
The present invention relates to compounds of Formula (I) inhibiting indoleamine 2,3-dioxygenase (IDO) and/or tryptophan 2,3-dioxygenase (TDO) enzymes. Further, their synthesis and their use as medicaments in inter alia cancer is disclosed.
This invention relates to piperidine derivatives of formula I wherein R
1
, R
2
, R
3
and R
4
are as defined herein useful in the treatment of a variety of disorders, including those in which the modulation of CCR5 receptors is implicated. Disorders that may be treated or prevented by the present derivatives include HIV and genetically related retroviral infections (and the resulting acquired immune deficiency syndrome, AIDS), rheumatoid arthritis, solid organ transplant reject (graft vs. host disease), asthma and COPD.
PYRIDINE DERIVATIVES, PREPARATION AND THERAPEUTIC APPLICATION THEREOF
申请人:Barre Lionel
公开号:US20080021070A1
公开(公告)日:2008-01-24
The invention relates to compounds of formula (I):
Wherein Z, R
3
to R
9
are as described herein. The invention also relates to methods of preparation of compounds of formula (I) and intermediates thereof. The compounds of this invention are active at CB1 cannabinoid receptor site, and are therefore, useful as pharmaceutical agents in treating a variety of diseases caused by the effects of CB1 cannabinoid receptors.
1,5-DIARYLPYRROLE DERIVATIVES, PREPARATION METHOD THEREOF AND APPLICATION OF SAME IN THERAPEUTICS
申请人:BARTH Francis
公开号:US20080015245A1
公开(公告)日:2008-01-17
The invention relates to compounds having formula (I):
Wherein X, R
1
, R
2
, R
3
, R
4
, R
5
and R
6
are as defined herein. The invention also relates to a method of preparing said compounds and to die application thereof in therapeutics.